-

  • ATX
    A10BD03

  • ,

  • , , . ( ).

    ( CYP2C8) 600 2 Css 2 . , CYP2C8 .

    CYP2C8 .

    ( CYP2C8) 600 / 65%. , CYP2C8, .

    Cmax AUC 18% (90% CI: 11% - 26%) 15% (90% CI: 8% - 23%), , .

    , , , .

    , S(-)- ( CYP2C9).

    .

    ( ) , , CYP3A4.

    + , .

    , ( . . ) , ( , ).

    / , , ( , 48 ).

    ,

    ( ), β2-, , , ; , .. .

    . .

  • (4 /500 ) , , , 4 500 . 1 /500 4 /500 .

    AUC . , Cmax - 209 /, 270 /, Cmax - 762 /, 909 /; max - 2.56 0.98 - 3.96 , 3 .

    4 8 99%. Cmax 1 . .

    AUC, Cmax ( 20-28%) max (1.75 ).

    , . .

    max 2.5 , 500 850 50-60%. . , , 20-30% .

    , . Css 24-48 , , 1 /. Cmax 4 /, .

    . 850 max 40% AUC - 25%, max 35 . .

    Vd 14 , - 3 /. - 99.8%, . 1-2

    . . Cmax , Cmax . , , .

    Vd 63 276 .

    , . N- , . .

    in vitro , CYP2C8 - CYP2C9.

    in vitro CYP1A2, CYP2A6, CYP2C19, CYP2D6, CYP2E1, CYP3A CYP4A , , in vivo , 450. In vitro CYP2C8 ( - 18 ) CYP2C9 ( - 50 ). in vivo , CYP2C9.

    . - .

    3 /, T1/2 3-4 . 1-2 2/3 , 25% . , . T1/2 130 , . , (), , , 5 .

    . 400 /. T1/2 6.5 .

    , .

    , .

    ( -) Cmax AUC 2-3 , .

    , , , T1/2 , .